US2024197722A1PendingUtilityA1

Anticancer composition inducing cell senescence and cell death

Assignee: OSTEONEUROGEN INCPriority: Apr 20, 2021Filed: Apr 14, 2022Published: Jun 20, 2024
Est. expiryApr 20, 2041(~14.8 yrs left)· nominal 20-yr term from priority
A61K 31/352A61P 35/02A61P 35/00A61K 31/496A23L 33/10
57
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Claims

Abstract

The present invention relates to an anticancer composition containing as an active ingredient a compound inducing cell senescence and apoptosis. The compound of the present invention can discriminate cancer cells and normal cells and induce both cell senescence and apoptosis in a cancer cell-specific manner. Thus, the compound does not need the attachment of any cancer cell-specific targeting substance thereto, can minimize the frequent adverse effects caused by the attack of anticancer agents on normal cells, and exhibits a potent anticancer effect on the basis of the aforementioned dual action.

Claims

exact text as granted — not AI-modified
1 . A method for inhibiting or treating or ameliorating tumor or cancer disease in a subject in need thereof, comprising:
 administering an effective amount of a compound represented by Chemical Formula 1 below or a salt thereof as an active ingredient to a subject in need thereof:   
       
         
           
           
               
               
           
         
         wherein in Chemical Formula 1 above, 
         R 1  is a C 1-5  alkyl, a C 5-6  cyclic alkyl, a C 5-6  cyclic alkyl containing at least one heteroatom of O or N, a C 6-12  aryl or a C 5-6  heteroaryl containing at least one heteroatom of O or N, 
         wherein R 2  is hydrogen, ethyl, acetyl, acetoxy, carboxy, benzoyloxy or 3,4,5-trihydroxybenzoyloxy, 
         wherein R 3  is hydrogen, hydroxy, methyl, methoxy, acetoxy, carboxy or benzoyloxy, 
         wherein R 4  is hydrogen, hydroxy, methyl, methoxy, acetoxy, carboxy or benzoyloxy, and 
         wherein R 5  is hydrogen, hydroxy, methyl, methoxy, acetoxy, carboxy or benzoyloxy. 
       
     
     
         2 . The method of  claim 1 , wherein R 1  is methyl, ethyl, cyclopentyl, cyclohexyl or phenyl. 
     
     
         3 . The method of  claim 1 , wherein R 1  is methyl,
 wherein R 2  is hydrogen,   wherein R 3  is hydrogen, hydroxy or methoxy,   wherein R 4  is hydroxy or methoxy, and   wherein R 5  is hydrogen, hydroxy or methoxy.   
     
     
         4 . The method of  claim 1 , wherein the compound is represented by any one of Chemical Formulas 2 to 5 below: 
       
         
           
           
               
               
           
         
       
     
     
         5 . The method of  claim 1 , wherein the cancer is blood cancer or solid cancer. 
     
     
         6 . The method of  claim 5 , wherein the blood cancer is leukemia, malignant lymphoma, multiple myeloma or aplastic anemia. 
     
     
         7 . The method of  claim 5 , wherein the solid cancer is brain tumor, benign astrocytoma, malignant astrocytoma, pituitary adenoma, meningioma, brain lymphoma, oligodendroglioma, craniopharyngioma, ependymoma, brainstem tumor, head and neck tumor, laryngeal cancer, oropharyngeal cancer, nasal cancer, nasopharyngeal cancer, salivary gland cancer, hypopharyngeal cancer, thyroid cancer, oral cancer, chest tumor, small cell lung cancer, non-small cell lung cancer, thymus cancer, mediastinal tumor, esophageal cancer, breast cancer, male breast cancer, abdominal tumor, stomach cancer, liver cancer, gallbladder cancer, biliary tract cancer, pancreatic cancer, small intestine cancer, colon cancer, anal cancer, bladder cancer, kidney cancer, male genital tumor, penile cancer, prostate cancer, female genital tumor, cervical cancer, endometrial cancer, ovarian cancer, uterine sarcoma, vaginal cancer, female external genital cancer, female urethral cancer or skin cancer. 
     
     
         8 . The method of  claim 1 , wherein the compound exhibits antitumor or anticancer activity by at least one action selected from the group consisting of:
 (i) inhibition of tumor or cancer cell-specific proliferation by the induction of replicative senescence (RS) and/or oncogene-induced senescence (OIS);   (ii) reversal of the tumor or cancer cell NAD/NADH ratio;   (iii) upregulation of tumor or cancer cell ROS; and   (iv) inducing tumor or cancer cell-specific apoptosis.   
     
     
         9 - 24 . (canceled) 
     
     
         25 . The method of  claim 1 , wherein the compound or a salt thereof is administered as a pharmaceutical composition, a quasi drug composition or a food composition.

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